science and technology

Azo derivatives of monoterpenes as anti-Helicobacter pylori agents: from synthesis to structure-based target investigation

By pubs.rsc.org
Published On ::

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00511B, Research Article
Open Access
Francesco Melfi, Marialuigia Fantacuzzi, Simone Carradori, Ilaria D'Agostino, Alessandra Ammazzalorso, Noemi Mencarelli, Marialucia Gallorini, Mattia Spano, Paolo Guglielmi, Mariangela Agamennone, Sazan Haji Ali, Ali Al-Samydai, Francesca Sisto
Monoterpene-derived azo benzenes showed selective antibacterial activity against Helicobacter pylori with a safe profile. An in silico investigation highlighted the inosine 5'-monophosphate dehydrogenase enzyme as the putative target.
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Recent advances from computer-aided drug design to artificial intelligence drug design

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00522H, Review Article
Keran Wang, Yanwen Huang, Yan Wang, Qidong You, Lei Wang
CADD and AIDD contribute to the drug discovery.
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Medicinal chemistry-based perspective on thiophene and its derivatives: Exploring the structural insights to discover plausible druggable leads

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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00450G, Review Article
Shikha Thakur, Devendra Kumar, shivani jaiswal, Kapil Kumar Goel, Pramod Rawat, Vivek Srivastava, Sonia Dhiman, Hemant R Jadhav, Ashish Ranjan Dwivedi
Thiophene is a privileged pharmacophore in medicinal chemistry owing to its diversified biological attributes. The thiophene moiety has been ranked 4th in US FDA drug approval of small drug molecules,...
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A decade of pyridine-containing heterocycles in US FDA approved drugs: a medicinal chemistry-based analysis

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00632A, Review Article
Ashish Ranjan Dwivedi, Shivani Jaiswal, Deepak Kukkar, Roshan Kumar, Thakur Gurjeet Singh, Mahendra Pratap Singh, Abhay M. Gaidhane, Sorabh Lakhanpal, K. Nagendra Prasad, Bhupinder Kumar
The present review is a concerted effort to cover drugs bearing pyridine rings approved in the last decade, and it provides thorough discussion and commentary on their pharmacokinetics and pharmacodynamics together with in-depth structural analysis.
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Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00579A, Research Article
Open Access
Cecilia C. Ayala-Aguilera, Yang Ge, Álvaro Lorente-Macías, Benjamin N. Jones, Catherine Adam, Neil O. Carragher, Asier Unciti-Broceta
A ligand-centred strategy combined with phenotypic screening was used to develop novel antiproliferative inhibitors against oesophageal cancer and identified a lead compound that induces potent anticancer activity and inhibits Aurora kinase A.
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Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00621F, Research Article
Chunfei Zhang, Yixin Liu, Xiao Zhang, Chunping Wan, Zewei Mao
A series of novel benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.
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S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00619D, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Marina Perieteanu, Tayner Rodriguez Garzon, Leah M. C. McGee, Abedawn I. Khalaf, Colin J. Suckling, Rebecca Beveridge, Vicky M. Avery, Fraser J. Scott
25 S-MGBs, including those bearing an amidine tail group, were investigated for their antiplasmodial, in vitro activity against 3D7 and Dd2 strains of P. falciparum. Several potent, and selective, hit compounds were identified.
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Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00555D, Research Article
Shenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E. Tollefson, Karoly Toth, Peng Zhan, Xinyong Liu
The continuous mutational nature of SARS-CoV-2 and its inter-species' similarities emphasize the urgent need to design and develop more direct-acting antiviral agents against highly infectious variants.
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Advances in antibacterial agents for Mycobacterium fortuitum

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00508B, Review Article
Carlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando Fumagalli
This review presents the recent findings on antibacterial agents against Mycobacterium fortuitum and reveals the most promising and effective chemical frameworks to inspire the development of new drugs.
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A novel approach for the synthesis of the cyclic lipopeptide globomycin

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00685B, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Samantha J. Bann, Stephen A. Cochrane
Lipid swapping: a new approach for the synthesis of globomycin that allows for facile lipid diversification.
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Design, synthesis, and biological evaluation of pyrazole–ciprofloxacin hybrids as antibacterial and antibiofilm agents against Staphylococcus aureus

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00623B, Research Article
Ojaswitha Ommi, Priyanka Sudhir Dhopat, Shashikanta Sau, Madhu Rekha Estharla, Srinivas Nanduri, Nitin Pal Kalia, Venkata Madhavi Yaddanapudi
A series of pyrazole–ciprofloxacin hybrids were designed, synthesized, and tested for antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Mycobacterium tuberculosis, aiming to combat antibiotic resistance.
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Novel quinoxaline-derived derivatives: design, synthesis, bioactive evaluation, SARs and preliminary antibacterial mechanism

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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00670D, Research Article
Yuting Liu, Pengju Yang, Yunyun Zhou, Zhiwen Zhou
In the current study, we have designed and prepared a series of quinoxaline-based compounds, which were derived from o-phenylenediamine. Among which, compounds 5m-p displayed good to moderate antibacterial activity with...
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Design and synthesis of (E)-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase

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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00373J, Research Article
YongLai Jiao, Jie Zhong, Jin-Fang Xu, Shaobo Ning, Taigang Liang, Mingzhu Zhao, Jian Zhang
The mitotic kinase Aurora A, a pivotal regulator of cell cycle, is overexpressed in various cancers and has emerged as one of the most promising targets for anticancer drug discovery....
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Metal-free synthesis of N-fused quinazolino-quinazoline-diones as a MALAT1 RNA triple helix intercalator

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00614C, Research Article
Vijay Babu Pathi, Pranotosh Das, Abhyuday Guin, Manish Debnath, Biswadip Banerji
The development of chemical scaffolds that target highly conserved MALAT1 RNA received attention due to its significance in splicing, nuclear organization, and gene expression in disease progression pathways.
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Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00663A, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Václav Pflégr, Klára Konečná, Jiřina Stolaříková, Jan Ősterreicher, Ondřej Janďourek, Martin Krátký
Linking pyridine-4-carbohydrazide to other antimicrobial agents via oxocarboxylic acids significantly enhances efficacy against mycobacteria with promising selectivity and safety profiles.
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Synthesis of cationic N-acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of N-acylation's role in membrane-disrupting activity

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00626G, Research Article
Aleena Pious, Vignesh Venkatasubramanian, Dharshini Karnan Singaravelu, Subburethinam Ramesh, Fuad Ameen, Anbazhagan Veerappan
Lipidation modulates the Gram-selective antibacterial activity of QPyNATh.
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Synthesis, in silico and bio-evaluation studies of new isothiocyanate derivatives with respect to COX inhibition and H2S release profiles

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00495G, Research Article
Yakup Berkay Yilmaz, Tuğba Güngör, Serhat Dönmez, Hazal Nazlıcan Atalay, Pınar Siyah, Serdar Durdağı, Mehmet Ay, Tugba Boyunegmez Tumer
New isothiocyanate derivatives (I1–3 and I1a–e) were synthesized and screened for their anti-inflammatory activities and H2S-releasing capacities. Compounds I1 and I1c demonstrated the most potent and selective COX-2 inhibition.
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meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells

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Published On ::

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00601A, Research Article
Open Access
Brém Balázs, Bianca Stoean (Vasile), Éva Molnár, Eva Fischer-Fodor, Ovidiu Bălăcescu, Raluca Borlan, Monica Focsan, Adriana Grozav, Patriciu Achimaş-Cadariu, Emese Gál, Luiza Gaina
New meso-substituted AB3-type phenothiazinyl porphyrins and ferrocenylvinyl phenothiazinyl porphyrin were synthesised by Suzuki–Miyaura and Mizoroki–Heck cross-coupling reactions, respectively.
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Generation and capture of naphthoquinonynes: a new frontier in the development of trypanocidal quinones via aryne chemistry

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00558A, Research Article
Laura P. R. Figueroa, Renato L. de Carvalho, Renata G. Almeida, Esther R. S. Paz, Emilay B. T. Diogo, Maria H. Araujo, Warley S. Borges, Victor F. S. Ramos, Rubem F. S. Menna-Barreto, James M. Wood, John F. Bower, Eufrânio N. da Silva Júnior
This article presents A-ring functionalized quinones via a modern and efficient new strategy involving the generation and capture of benzyne quinones and their evaluation against Trypanosoma cruzi.
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Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00553H, Research Article
Stefano Tomassi, Benito Natale, Michele Roggia, Luisa Amato, Caterina De Rosa, Carminia Maria Della Corte, Emma Baglini, Giorgio Amendola, Anna Messere, Salvatore Di Maro, Elisabetta Barresi, Federico Da Settimo, Maria Letizia Trincavelli, Fortunato Ciardiello, Sabrina Taliani, Floriana Morgillo, Sandro Cosconati
Non-small cell lung cancer (NSCLC), the leading cause of cancer-related mortality worldwide, poses a formidable challenge due to its heterogeneity and the emergence of resistance to targeted therapies.
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Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

By pubs.rsc.org
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00637B, Review Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Qiang Yang, Yunpeng Liu
Fc-glycan-specific ADC is a significant advance in site-specific ADCs for cancer therapy. Notably, JSKN003 and IBI343 have demonstrated promising results in phase 1 clinical trials and are advancing into phase 3 studies.
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Light enhanced cytotoxicity and antitumoral effect of a ruthenium-based photosensitizer inspired from natural alkaloids

By pubs.rsc.org
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00600C, Research Article
Open Access
Gennaro Sanità, Maria Laura Alfieri, Barbara Carrese, Serena Damian, Vincenza Mele, Gaetano Calì, Brigida Silvestri, Sebastiano Marra, Susan Mohammadi, Giuseppina Luciani, Paola Manini, Annalisa Lamberti
Biological assays carried out on melanoma and breast cancer cells highlighted the role of light in boosting the cytotoxic effect of a ruthenium complex featuring a dihydroisoquinoline ligand suggesting applications in photodynamic therapy.
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Property-based optimisation of PROTACs

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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00769G, Opinion
James Scott, Iacovos Michaelides, Markus Schade
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical...
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3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships

By pubs.rsc.org
Published On ::

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00597J, Research Article
Albert Michael Crider, Audrey Hospital, Karin Sandoval, William Neumann, Stephen Kukielski, Lejla Garic, Kristen Ingold, Matthew Dunahoo, Khush Srabony, Rafael Frare, Olivia Slater, Nathan Peel, Maria Kontoyianni, Ken Witt
Somatostatin receptor-4 (SST4) is a therapeutic target for several conditions, including Alzheimer’s disease, seizures, neuropsychiatric disorders, and pain. Our previous work on 1,2,4-triazole derivatives led to enhanced SST4 binding affinity,...
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A practical guide for the assay-dependent characterisation of irreversible inhibitors

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00707G, Review Article
Lavleen K. Mader, Jessica E. Borean, Jeffrey W. Keillor
Kinetic evaluations for assay dependent characterization of irreversible inhibitors.
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SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction

By pubs.rsc.org
Published On ::

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00722K, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Maria Cristina Lomuscio, Nicola Corriero, Vittoria Nanna, Antonio Piccinno, Michele Saviano, Rosa Lanzilotti, Carmen Abate, Domenico Alberga, Giuseppe Felice Mangiatordi
Developing sigma-1 receptor (S1R) modulators is considered a valuable therapeutic strategy to counteract neurodegeneration, cancer progression, and viral infections, including COVID-19. In this context, in-silico tools capable of accurately predicting...
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Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00724G, Research Article
Zhengxiao Huang, Hongjie Chen, Xiao Zhang, Ruirui Wang, Chunyan Hu, Zewei Mao
A series of novel azole derivatives containing 1,2,3-triazole have been synthesized with good antifungal effects on sensitive and drug-resistant C. albicans.
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Adjuvant strategies to tackle mcr-mediated polymyxin resistance

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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00654B, Review Article
Madison R. Nuske, Junlang Zhong, Renjie Huang, Vijayalekshmi Sarojini, Jack L. Y. Chen, Christopher J. Squire, Mark A. T. Blaskovich, Ivanhoe K. H. Leung
The emergence of the mobile colistin resistance (mcr) gene is a significant threat contributing to the worldwide antibiotic resistance crisis. This review discusses adjuvant strategies to restore polymyxin sensitivity in these resistant bacteria.
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542: Breaking Up with CSS-in-JS, Mastodon, and Stories on the Web

By shoptalkshow.com
Published On :: Mon, 21 Nov 2022 08:00:51 +0000

We're talking CSS-in-JS, Token CSS, Matuzo being suspended from Twitter, trying out Mastodon, testing out stable diffusion, stories on the web, and Jake Albaugh's new social network.


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543: Zach Leatherman on Eleventy, Mastodon, Twitter, and is-land

By shoptalkshow.com
Published On :: Tue, 29 Nov 2022 16:30:32 +0000

Zach Leatherman talks with us about what's new with Eleventy, setting up on Mastodon, what's happened with Twitter, and is-land.


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544: Feedback, RSS Talk, Arc Brower, and Product Talk

By shoptalkshow.com
Published On :: Mon, 05 Dec 2022 08:15:42 +0000

Getting feedback for what you're building or writing, RSS feed reminiscing, Arc browser thoughts, products that didn't make that should have.


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545: Arc Browser with Nate Parrott

By shoptalkshow.com
Published On :: Mon, 12 Dec 2022 09:49:46 +0000

Nate Parrott from The Browser Company of New York stops by to talk about Arc - including the history of Arc, how boosts work, building out dev features, how they deciding on what features to build, and feedback from Dave and Chris on Arc.


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546: Ryan Dahl and Deno

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Published On :: Mon, 19 Dec 2022 09:11:01 +0000

Ryan Dahl stops by to talk about Node, Deno, JavaScript, testing, V8, and thoughts around getting started with Deno.


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547: WordPress and GraphQL with Jason Bahl

By shoptalkshow.com
Published On :: Mon, 09 Jan 2023 09:31:13 +0000

Jason Bahl joins the show to talk about the GraphQL and WordPress connection, his work on WP GraphQL plugin, Faust and Atlas from WP Engine, Jamstack and Wordpress, and more.


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548: Infinite Canvas, Luro + Figma, and Scraping or Crawling

By shoptalkshow.com
Published On :: Mon, 16 Jan 2023 10:41:42 +0000

What's going to happen to homework with AI? Thoughts on infinite canvas which leads into Luro and Sigma integration, and Chris gets nerdsniped and tries to scrap (or should he crawl?) websites for data.


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549: Ben Ubois of Feedbin

By shoptalkshow.com
Published On :: Mon, 23 Jan 2023 08:43:45 +0000

Ben Ubois is the founder of Feedbin, the RSS reader of choice for Dave and Chris. What influenced the creation of Feedbin, the state of RSS in 2023, curating your RSS feed, and subscribing to newsletters in Feedbin.


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550: Sanity with Simen Svale Skogsrud and Espen Hovlandsdal

By shoptalkshow.com
Published On :: Mon, 30 Jan 2023 10:11:40 +0000

Simen and Espen from Sanity stop by to talk about the origins of Sanity, how Sanity Studio works, good use cases for Sanity, how Sanity does real time updates, what Groq is, and where to start with Sanity.


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551: PlanetScale with Iheanyi Ekechukwu and Mike Coutermarsh

By shoptalkshow.com
Published On :: Mon, 06 Feb 2023 19:44:27 +0000

Iheanyi Ekechukwu and Mike Coutermarsh talk about PlanetScale, what Vitess is, if PlanetScale is for both side and big projects, what read only regions are, what schema changes are, and how PlanetScale compares to other projects.


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552: Do You Want to Build a JS Framework? ☃️ CSS Wishlist for 2023

By shoptalkshow.com
Published On :: Mon, 13 Feb 2023 10:07:40 +0000

Austin power updates, what do you need if you want to build a new JavaScript framework, and what do we hope CSS brings in 2023?


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553: TypeScript, DX, GripeScript, and Astro v2 with Fred Schott

By shoptalkshow.com
Published On :: Mon, 20 Feb 2023 10:37:22 +0000

Fred Schott stops by to talk about TypeScript, what DX means in 2023, a bit of GripeScript, and being transparent about what Astro is good at, and what it's not.


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554: Jamstack Thoughts with Brian Rinaldi

By shoptalkshow.com
Published On :: Mon, 27 Feb 2023 20:50:01 +0000

Brian Rinaldi joins us to talk about the state of Jamstack in 2023, acronym confusion, SPA confusion, developing common tools of understanding, why Netlify bought Gatsby, and the state of developer conferences.


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555: React Documentary, Front of the Front End, Fast Fallacy, and Best Practices

By shoptalkshow.com
Published On :: Mon, 06 Mar 2023 09:39:37 +0000

Reacting to the React.js documentary, is there still jobs for front of the front end anymore? The fast fallacy in frameworks, best practices, dealing with too much or too little isolation, and AI test generation.


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556: Andrey Sitnik and Using OKLCH for Color

By shoptalkshow.com
Published On :: Mon, 13 Mar 2023 16:38:12 +0000

Andrey Sitnik from Evil Martians talks with us about why OKCLH is the best way forward for color on the web, how to incorporate it into design systems, getting your designers to use OKCLH, and what kind of fallback support is needed.


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557: ChatGPT, Conferences, Fidgets on the Web, and Modern CSS in Real Life

By shoptalkshow.com
Published On :: Mon, 20 Mar 2023 07:01:51 +0000

When will AI be able to tell you the risk / reward of cleaning up trees? Are conferences back? Bringing fidgets to the web, internet as an anxiety machine, and Chris is working on talk on modern CSS in real life.


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558: Esoteric Weird Content Editable Problems with Kristin Valentine

By shoptalkshow.com
Published On :: Mon, 27 Mar 2023 07:34:54 +0000

Kristin Valentine from Vox joins the show to talk about text editor CMS fun across multiple sites, Vox's Chorus, The Verge redesign, sharing Design Systems, theming articles, and a fun new game called "Can Your Text Editor Do This??"


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559: Fidget Apps, Coding with AI, Dialog Element Navs, Getting Rid of CSS

By shoptalkshow.com
Published On :: Mon, 03 Apr 2023 07:14:35 +0000

Is there still any value in specializing in front-of-the-frontend dev? Would you ever use the dialog element for a mobile navigation? Why did CodePen decide to use Go for its GraphQL server?


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560: Oh Biscuits! Cascade Layers, Block Links, Emoji Lists, and more CSS!

By shoptalkshow.com
Published On :: Mon, 10 Apr 2023 08:53:57 +0000

After a brief visit from Hip Hop Dad Dave, we're talking cascade layers updates, block link practices, search element getting dropped, how to use cite, emoji list accessibility, scrollbar state, and trigonometric functions in CSS.


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561: Web Perf News, Web Sommelier, Data Analytics, and Passkeys

By shoptalkshow.com
Published On :: Mon, 17 Apr 2023 08:00:36 +0000

Topics for this one include how do you learn about web performance news? Do you need a web components sommelier? Our thoughts on Syntax going to Sentry, and being able to focus on the things you want to focus on. Passkeys, Arc split screen, and vibe driven development.


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562: Podcast Apps, Zaraz, Future CSS Thoughts, and Arc

By shoptalkshow.com
Published On :: Mon, 24 Apr 2023 08:01:44 +0000

What if Taylor Swift lyrics hold the answers to web dev questions? Podcast app thoughts, using Cloudflare Zaraz, what we're excited about with CSS, Arc browser updates, and are we even developers or are we specialized systems whisperers?


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563: Getting Pulled by the Algorithm, AI Training Data, and SVG Drawing

By shoptalkshow.com
Published On :: Mon, 01 May 2023 08:51:30 +0000

There's a special guest on the show who takes aim at the billionaires in web dev, do we know better than the algorithm for news, why is AI training data such a secret, Chris and Dave discover JetBrains, monorepo struggles, and SVG drawing tools.


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